CN102574812B - 新型苯并咪唑衍生物及它们作为fxr激动剂的用途 - Google Patents

新型苯并咪唑衍生物及它们作为fxr激动剂的用途 Download PDF

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Publication number
CN102574812B
CN102574812B CN201080043283.8A CN201080043283A CN102574812B CN 102574812 B CN102574812 B CN 102574812B CN 201080043283 A CN201080043283 A CN 201080043283A CN 102574812 B CN102574812 B CN 102574812B
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China
Prior art keywords
difluoro
phenyl
chloro
benzimidazole
benzimidazol
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Expired - Fee Related
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CN201080043283.8A
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Chinese (zh)
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CN102574812A (zh
Inventor
格雷戈里·马丁·本森
康拉德·辈莱切
冯松
尤伟·格雷瑟
贝恩德·库恩
勒内·E·马丁
让-马克·普朗谢
汉斯·里斯特
马库斯·鲁道夫
斯文·泰勒
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201080043283.8A 2009-09-29 2010-09-27 新型苯并咪唑衍生物及它们作为fxr激动剂的用途 Expired - Fee Related CN102574812B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09171700 2009-09-29
EP09171700.9 2009-09-29
PCT/EP2010/064217 WO2011039130A1 (en) 2009-09-29 2010-09-27 New benzimidazole derivatives and their use as fxr agonists

Publications (2)

Publication Number Publication Date
CN102574812A CN102574812A (zh) 2012-07-11
CN102574812B true CN102574812B (zh) 2016-03-30

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CN201080043283.8A Expired - Fee Related CN102574812B (zh) 2009-09-29 2010-09-27 新型苯并咪唑衍生物及它们作为fxr激动剂的用途

Country Status (12)

Country Link
US (1) US8309581B2 (enrdf_load_stackoverflow)
EP (1) EP2483247A1 (enrdf_load_stackoverflow)
JP (1) JP5503007B2 (enrdf_load_stackoverflow)
KR (1) KR101477872B1 (enrdf_load_stackoverflow)
CN (1) CN102574812B (enrdf_load_stackoverflow)
AU (1) AU2010303146A1 (enrdf_load_stackoverflow)
BR (1) BR112012006986A2 (enrdf_load_stackoverflow)
CA (1) CA2772815A1 (enrdf_load_stackoverflow)
IL (1) IL218037A0 (enrdf_load_stackoverflow)
IN (1) IN2012DN01234A (enrdf_load_stackoverflow)
MX (1) MX2012002479A (enrdf_load_stackoverflow)
WO (1) WO2011039130A1 (enrdf_load_stackoverflow)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3043865B1 (en) 2013-09-11 2020-11-04 Institut National de la Sante et de la Recherche Medicale (INSERM) Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
CN108072684B (zh) * 2016-11-11 2020-06-16 中国科学院广州生物医药与健康研究院 法尼醇x受体的新配体及其筛选方法和应用
WO2018153933A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar agonist with a fxr agonist
CN110944635A (zh) 2017-03-30 2020-03-31 国家医疗保健研究所 用于减少附加体病毒的持久性和表达的方法和药物组合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101228152A (zh) * 2005-07-22 2008-07-23 赛诺菲-安万特 N-(杂芳基)-1-杂芳基烷基-1h-吲哚-2-羧基酰胺衍生物、其制备方法及其在制药中的应用
WO2008101586A1 (de) * 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate
CN101479249A (zh) * 2006-06-29 2009-07-08 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008291148B2 (en) * 2007-08-27 2011-03-17 F. Hoffmann-La Roche Ag Benzimidazole derivatives used as FXR agonists
ES2403592T3 (es) * 2007-11-15 2013-05-20 F. Hoffmann-La Roche Ag Nuevos derivados de bencimidazol y su empleo como agonsitas del FXR
JP5530445B2 (ja) * 2008-09-11 2014-06-25 エフ．ホフマン−ラ ロシュ アーゲー 新規ベンゾイミダゾール誘導体
WO2010043513A1 (en) * 2008-10-15 2010-04-22 F. Hoffmann-La Roche Ag New benzimidazole derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101228152A (zh) * 2005-07-22 2008-07-23 赛诺菲-安万特 N-(杂芳基)-1-杂芳基烷基-1h-吲哚-2-羧基酰胺衍生物、其制备方法及其在制药中的应用
CN101479249A (zh) * 2006-06-29 2009-07-08 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂
WO2008101586A1 (de) * 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate

Also Published As

Publication number Publication date
JP5503007B2 (ja) 2014-05-28
EP2483247A1 (en) 2012-08-08
IL218037A0 (en) 2012-04-30
CA2772815A1 (en) 2011-04-07
US8309581B2 (en) 2012-11-13
CN102574812A (zh) 2012-07-11
BR112012006986A2 (pt) 2016-04-12
AU2010303146A1 (en) 2012-04-19
KR101477872B1 (ko) 2014-12-30
HK1171746A1 (zh) 2013-04-05
KR20120063536A (ko) 2012-06-15
WO2011039130A1 (en) 2011-04-07
IN2012DN01234A (enrdf_load_stackoverflow) 2015-05-15
US20110077273A1 (en) 2011-03-31
MX2012002479A (es) 2012-03-26
JP2013505977A (ja) 2013-02-21

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